Medmain, also known as 2-methyl-3-ethyl-5-dimethylaminoindole, is a serotonin receptor modulator, convulsant, and indole derivative related to the neurotransmitter serotonin. It has low-potency serotonin antagonist or partial agonist activity, with low affinity for serotonin 5-HT1 and 5-HT2 receptors (IC50Tooltip half-maximal inhibitory concentration = >1,000 nM) but greater activity against the serotonin receptors in the rat stomach fundus strip (KB = 50 nM) (thought to represent the serotonin 5-HT2B receptor). Owing to its convulsant activity, medmain was tested in animals but not in humans. The drug was described and studied by E. Shaw and Dilworth Woolley in the 1950s. A derivative, 1-methylmedmain, is also known, and has similar potency as a serotonin antagonist but lacks the convulsant activity of medmain. Other analogues of medmain have been explored as well, but none had improved activity at the rat fundus strip serotonin 5-HT2B receptor compared to medmain and 1-methylmedmain.
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